产品介绍 SC144 是首创的 gp130 (IL6-beta) 抑制剂。SC144 结合 gp130，诱导 gp130 磷酸化(S782) 和去糖基化，消除 Stat3 磷酸化和核易位，进一步抑制下游靶基因的表达。SC144 对 gp130 配体触发的信号转导有明显的抑制作用。SC144 诱导人卵巢癌细胞凋亡。 SC144是gp130抑制剂，对NCI/ADR-RES和HEY细胞系的IC50值分别为0.43 μmol/L和0.88 μmol/L。 SC144是第一个gp130小分子抑制剂，具有口服活性，应用于卵巢癌治疗。在OVCAR-8和CAOV-3细胞中，SC144呈时间和剂量依赖性地显著增加gp130磷酸化（S782）。由于Stat3的组成性激活是由细胞外gp130配体维持，磷酸化的增加可进一步抑制Stat3信号传导通路。此外，SC144促使大量上述细胞凋亡。 除了对gp130的作用，据报道，SC144可以直接结合并稳定癌细胞中的IL-24。此外，SC144也对细胞周期紊乱和凋亡诱导有效。 SC144也可以靶向其它细胞蛋白，参与多种潜在的分子机制。SC144的抗癌功效可能是上述作用的综合结果。 SC144 hydrochloride has been used: as a glycoprotein 130 (gp130) inhibitor to evaluate the effect of bazedoxifene on interleukin (IL-6) mediated cell viability in pancreatic cancer cells as a gp130 inhibitor to study its effects on signal transducer and activator of transcription 3 (STAT3) activation in mesenchymal precursor cells (KMM) cells as an interleukin 6 signal transducer (IL-6ST) inhibitor in media to test its ability to block serum-induced migration/invasion
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SC144
CAS number：895158-95-9 molecular formula：C16H11FN6O
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Specs
| Chinese alias | - | ||
| English alias | N'-(7-fluoropyrrolo[1,2-a]quinoxalin-4-yl)pyrazine-2-carbohydrazide | 2-(7-Fluoropyrrolo[1,2-a]quinoxalin-4-yl)hydrazide-2-pyrazinecarboxylic acid | 2-Pyrazinecarboxylic acid, 2-(7-fluoropyrrolo[1,2-a]quinoxalin-4-yl)hydrazide | ||
| CAS number | 895158-95-9 | molecular formula | C16H11FN6O |
| molecular weight | 322.3 g/mol | Exact mass | ≥98% |
| PSA | 84.200 Ų | logp | 2.600 |
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